GSK 2833503A

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Cat.No. 6497 - GSK 2833503A | C18H21ClFN3OS | CAS No. 1366234-01-6
Description: Potent and selective TRPC6 and TRPC3 antagonist
Chemical Name: [2-[(4-Chloro-2-fluorophenyl)amino]-5-methyl-4-thiazolyl][(2S,3S)-2,3-dimethyl-1-piperidinyl]methanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for GSK 2833503A

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cells in vitro and in cardiomyocytes.

Technical Data for GSK 2833503A

M. Wt 381.89
Formula C18H21ClFN3OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1366234-01-6
PubChem ID 71818575
InChI Key ODUIXUGXPFKQLG-QWRGUYRKSA-N
Smiles C[C@H]1CCCN(C(C2=C(SC(NC3=C(C=C(C=C3)Cl)F)=N2)C)=O)[C@H]1C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GSK 2833503A

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.19 100
ethanol 7.64 20

Preparing Stock Solutions for GSK 2833503A

The following data is based on the product molecular weight 381.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.62 mL 13.09 mL 26.19 mL
5 mM 0.52 mL 2.62 mL 5.24 mL
10 mM 0.26 mL 1.31 mL 2.62 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets for GSK 2833503A

Certificate of Analysis is currently unavailable on-line.
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References for GSK 2833503A

References are publications that support the biological activity of the product.

Washburn et al (2013) The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg.Med.Chem.Lett. 23 4979 PMID: 23886683

Seo et al (2014) Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy. Proc.Natl.Acad.Sci.U.S.A. 111 1551 PMID: 24453217


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Citations for GSK 2833503A

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